Ipatasertib free base · Synonyms: GDC-0068 | RG7440

Ipatasertib is an orally active, highly selective and ATP-competitive pan-Akt inhibitor.

For research use only. Not for human or veterinary use.

Target Organoid Akt Apoptosis

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

Ipatasertib structure

CAS No.: 1001264-89-6

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 585.00	BP-02343-250mg	In stock	Get quote
500 mg	USD 748.00	BP-02343-500mg	In stock	Get quote
1 g	USD 1,120.00	BP-02343-1g	In stock	Get quote
2 g	USD 1,980.00	BP-02343-10g	In stock	Get quote
5 g	Inquire	BP-02343-5g	In stock	Inquire

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Description

Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models.

Biological activity

Ipatasertib (GDC-0068, RG7440) is a novel, ATP-competitive and orally bioavailable Akt inhibitor with IC50 values of 5 nM, 18 nM and 8 nM for Akt1, Akt2 and Akt3, respectively. Ipatasertib (GDC-0068) demonstrates potent inhibition of all three Akt isoforms in biochemical assays, but poor inhibition of other AGC family kinases. Moreover, GDC-0068 selectively inhibits cell cycle progression and viability of cancer cell lines driven by PI3K/Akt signaling pathway, including those with defects in the tumor suppressor PTEN, oncogenic mutations in PIK3CA, and amplification of HER2. GDC-0068 (Ipatasertib) blocks the phosphorylation of multiple downstream targets of Akt in human cancer cell lines. GDC-0068 (RG7440) shows good oral exposure resulting in dose-dependent pharmacodynamic effects on downstream biomarkers and a robust anti-tumor response in xenograft models in which the PI3K-Akt-mTOR pathway is activated.

Identifiers

SMILES: CC(C)NC[C@@H](C(=O)N1CCN(CC1)C1=C2[C@H](C)C[C@@H](O)C2=NC=N1)C1=CC=C(Cl)C=C1
InChIKey: GRZXWCHAXNAUHY-NSISKUIASA-N

Specifications

MW (average): 457.9960
Formula: C₂₄H₃₂ClN₅O₂
CAS No.: 1001264-89-6
Physical state: Solid
Color: White to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO/water

Documents

References

[1]. Sun L, et al. Ipatasertib, a novel Akt inhibitor, induces transcription factor FoxO3a and NF-κB directly regulates PUMA-dependent apoptosis. Cell Death Dis. 2018 Sep 5;9(9):911.

[2]. Blake JF, et al. Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors. J Med Chem. 2012 Sep 27;55(18):8110-27.

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